(19) |
 |
|
(11) |
EP 0 340 662 A1 |
(12) |
EUROPEAN PATENT APPLICATION |
(43) |
Date of publication: |
|
08.11.1989 Bulletin 1989/45 |
(22) |
Date of filing: 28.04.1989 |
|
|
(84) |
Designated Contracting States: |
|
AT BE CH DE ES FR GB GR IT LI LU NL SE |
(30) |
Priority: |
05.05.1988 CH 1681/88
|
(71) |
Applicant: IBSA - INSTITUT BIOCHIMIQUE S.A. |
|
CH-6903 Lugano (CH) |
|
(72) |
Inventor: |
|
- Lualdi, Paolo
F-22070 Grandate (Como) (IT)
|
(74) |
Representative: Gervasi, Gemma, Dr. et al |
|
NOTARBARTOLO & GERVASI Srl
Viale Bianca Maria 33 20122 Milano 20122 Milano (IT) |
|
|
|
(54) |
Solid, water-soluble, pharmaceutical composition containing acetylcysteine |
(57) Solid, water-soluble pharmaceutical composition containing the following parts by
weight of the following components: 5-25 acetylcysteine, 70-85 xylitol, 0.5-1.2 sodium
saccharin bihydrated, 0.4-1.2 beta-carotene, 4-7.5 flavors.
[0001] The present invention relates to a solid, water-soluble, pharmaceutical composition
having as active principle acetylcysteine.
[0002] It is known that acetylcysteine (Index Nominum - 1987 - page 9) is a highly tolerable
drug possessing interesting pharmacological activities, predominant among which the
mucolytic one.
[0003] It is also known that acetylcysteine may be administered through all the customary
administration methods.
[0004] It is further known that the administration of acetylcysteine as a mucolytic is frequently
done "per os" using solid water-soluble pharmaceutical forms, which are dissolved
in water at the moment of use, such as e.g. powders, granules or effervescent tablets.
[0005] Similarly to many aliphatic thioderivatives, acetylcysteine has disagreable odor
and taste, which must be adequately masked. In the past many formulations have been
suggested in which attempts were made to mask the taste and odor of acetylcysteine
by the addition of sweetening and flavoring agents.
[0006] The problem of the palatability may be solved in a relatively satisfactory way by
using saccharose as a sweetening agent; however, the amount required is rather high
and inconvenient to diabetic patients as well as in all other instances in which it
is desirable to limit the assumption of high caloric substances.
[0007] Other sweetening agents do not have a sufficient masking capacity.
[0008] We have now found a particularly agreable and palatable solid, water-soluble, pharmaceutical
composition containing the following parts by weight of the following components:
5-25 acetylcysteine, 70-85 xylitol, 0.5-1.2 sodium saccharin bihydrated, 0.4-1-2 beta
carotene, 4-7.5 flavors.
[0009] Futhermore, the flavor presence permits also to adequately mask the acetylcysteine
odor.
[0010] The preferred embodiment according to the present invention is constituted by granules
and the preferred preparation consists of small bags of a non-toxic material, compatible
with the granules, impervious to air and humidity, containing the suitable dosage
unit. A typical example of a suitable material for said bags is represented by coupled
aluminium-polyethylene foils, the polyethylene being in contact with the dosage units.
Said dosage units are predetermined by the pharmacologist and the physician according
to known criteria, and each contains preferably 100, 200, 400, 600 mg of acetylcysteine.
[0011] The solid, water-soluble, pharmaceutical compositions according to the present invention
are prepared by methods known to the technician in the field, who has also knowledge
of the materials and apparatus required.
[0012] Typically, the preparation of a granular material according to the present invention
is carried out by first granulating xylitol with a water solution containing ca. 20%
beta carotene and 20% sodium saccharin bihydrated in a fluid bed granulator. To the
thus obtained granules there are then added in an external phase, acetylcysteine and
orange flavor consisting of deterpenized essential oils supported on arabic gum and
malto-dextrines, the essential oils representing approximately 18% by wt.
[0013] The thus prepared granules are distributed in small aluminium-polyethylene bags
in amounts corresponding to the predetermined dosage units.
[0014] Non-limitative examples of compositions according to the present invention are:
|
mg |
mg |
mg |
mg |
Acetylcysteine |
100 |
200 |
400 |
600 |
Xylitol |
1271 |
1171 |
1471 |
2166 |
Sodium saccharin bihydrated |
15 |
15 |
15 |
20 |
Beta carotene |
14 |
14 |
14 |
14 |
Orange flavor |
100 |
100 |
100 |
200 |
[0015] The pharmaceutical compositions according to the present invention have proved to
be chemically as well as organoleptically stable for at least two years at room temperature.
[0016] The palatalability tests have shown that the organoleptic characteristics of the
compositions according to the present invention are significantly better than the
ones possessed by the compositions sweetened with sorbitol, aspartame and similar
products.
1. A solid, water-soluble, pharmaceutical composition containing the following parts
by weight of the following components:
5-25 acetylcysteine, 70-85 xylitol, 0.5-1.2 sodium saccharin bihydrated, 0.4-1.2 beta
carotene and 4-7.5 flavors.
2. A pharmaceutical composition according to claim 1, in which each dosage unit consists
of water-soluble granules having the following composition : 100 mg acetylcysteine,
1271 mg xylitol, 15 mg sodium saccharin bihydrated, 14 mg beta carotene, 100 mg orange
flavor.
3. A pharmaceutical composition according to claim 1, in which each dosage unit consists
of water-soluble granules having the following composition: 200 mg acetylcysteine,
1171 mg xylitol, 15 mg sodium saccharin bihydrated, 14 mg beta carotene and 100 mg
orange flavor.
4. A pharmaceutical composition according to claim 1, in which each dosage unit consists
of water-soluble granules having the following composition: 400 mg acetylcysteine,
1471 mg xylitol, 15 mg sodium saccharin bihydrated, 14 mg beta carotene and 100 mg
orange flavor.
5. A pharmaceutical composition according to claim 1, in which each dosage unit consists
of water-soluble granules having the following composition: 600 mg acetylcysteine,
2166 mg xylitol, 20 mg sodium saccharin bihydrated, 14 mg beta carotene, 200 mg orange
flavor.
